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Inhibitory effects of xanthohumol and its synthetic derivatives on the activity and expression of matrix metalloproteinase (MMP)‐2 and MMP‐9
Author(s) -
Kang YouRa,
Lee Jong Suk,
Park Mi Hye,
Lee Yong Rok,
Park Jyung Rewng,
Kim JungAe
Publication year - 2008
Publication title -
the faseb journal
Language(s) - English
Resource type - Journals
SCImago Journal Rank - 1.709
H-Index - 277
eISSN - 1530-6860
pISSN - 0892-6638
DOI - 10.1096/fasebj.22.2_supplement.713
Subject(s) - xanthohumol , matrix metalloproteinase , chemistry , matrix metalloproteinase inhibitor , inhibitory postsynaptic potential , matrix metalloproteinase 9 , matrix (chemical analysis) , pharmacology , biochemistry , medicine , biology , key (lock) , ecology , chromatography
Previously, xanthohumol has been shown chemopreventive and antiangiogenic activities. Angiogenesis is an invasive process requiring proteolytic activities such as matrix metalloproteinases (MMPs) that are also important for the tumor cell invasion. In this study, we have examined whether xanthohumol and its synthetic derivatives L5, L6, and L7 inhibits MMP‐2 and MMP‐9 activities in HT1080 human fibrosarcoma cells. Xanthohumol and compound L7 induced 50% reduction in the cell viability at 15 μM and more than 100 μM, respectively. In contrast, compounds L5 and L6 did not affect the cell viability up to 100 μM concentrations. Xanthohumol inhibited the activity as well as secreted protein level of both MMP‐2 and MMP‐9 in a concentration‐dependent manner with very strong effect at 10 μM. The compounds L6 and L7 significantly reduced the activities and protein level of MMP‐2 and MMP‐9 at higher concentration of 50 μM. However, the compound L5 did not induce any change in MMP activities. In addition, xanthohumol and the derivative, L6 and L7 significantly inhibited HT1080 cell invasion. In a free radical scavenging activity test, xanthohumol and the derivatives L5, L6, and L7 did not scavenged DPPH radicals. Taken together, our results suggest that xanthohumol and its derivatives may be valuable compounds for inhibiting cancer cell invasion.